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Journal Articles

Structural and Biochemical Studies Confirming the Mechanism of Action of Asciminib, an Agent Specifically Targeting the ABL Myristoyl Pocket (STAMP)

Peter Schuld, PhD, Stephan Grzesiek, PhD, Johannes Schlotte, Judith M Habazettl, PhD, Wolfgang Jahnke, PhD, Louise Barys, MS, Sandra W Cowan-Jacob, PhD, Alice Loo, MS, Andrea Wiget, Paul W. Manley, PhD

Blood (2020) 136 (Supplement 1): 34–35.

https://doi.org/10.1182/blood-2020-140968

Published: 2020

Journal Articles

Comparison of the Profile of the AML Drug Midostaurin (Rydapt®) As a Kinase Inhibitor with Those of Its Predominant Primary Human Metabolites

Paul W Manley, Giorgio Caravatti, Pascal Furet, Johannes Roesel, Phi Tran, Trixie Wagner

Blood (2017) 130 (Supplement 1): 1383.

https://doi.org/10.1182/blood.V130.Suppl_1.1383.1383

Published: 2017

Journal Articles

ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Resistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia

Blood (2014) 124 (21): 398.

https://doi.org/10.1182/blood.V124.21.398.398

Published: 2014

Journal Articles

Clinical and Preclinical Characterisation Of The Metabolites Of The BCR-ABL Tyrosine Kinase Inhibitor Nilotinib

Paul W. Manley, Ph. D., Jürgen Mestan, Ph D, Jennifer Sheng, Ph D, Phi Tran, M Sc, Mark Kagan, Ph D

Blood (2013) 122 (21): 4011.

https://doi.org/10.1182/blood.V122.21.4011.4011

Published: 2013

Journal Articles

Assessment of Clinical Safety and Estimate of Survival in Iraqi Patients with Chronic Myeloid Leukemia Switched From Glivec (β-Crystalline Form of Imatinib Mesylate) to an α-Crystalline Copy of Imatinib Mesylate

Marc Botteman, MSc, MA, Matthew Magestro, Alaa Fadhil Alwan, MD, Paul W Manley, PhD, Oleg Zernovak, MD, Richard C. Woodman

Blood (2012) 120 (21): 4439.

https://doi.org/10.1182/blood.V120.21.4439.4439

Published: 2012

Journal Articles

Potentiation of the Effects of Nilotinib by Combination with Plerixafor in a Mouse Model of BCR-ABL-Positive Residual Disease

Ellen L Weisberg, Ph.D., Paul W. Manley, Ph. D., Andrew L. Kung, MD, PhD, James D. Griffin, MD

Blood (2011) 118 (21): 2737.

https://doi.org/10.1182/blood.V118.21.2737.2737

Published: 2011

Journal Articles

Fingolimod (FTY720) Inhibits BCR-ABL Signaling Allosterically by Binding to the Myristate Binding Site

Paul W. Manley, Ph. D., Sandra W. Cowan-Jacob, Robert Cozens, Gabriele Fendrich, Wolfgang Jahnke, Johannes L Roesel, Doriano Fabbro

Blood (2011) 118 (21): 2746.

https://doi.org/10.1182/blood.V118.21.2746.2746

Published: 2011

Journal Articles

Nilotinib, in Comparison to Both Dasatinib and Imatinib, Possesses a Greatly Prolonged Residence Time When Bound to the BCR-ABL Kinase SH1 Domain

Paul W. Manley, Ph. D., Sandra W. Cowan-Jacob, Gabriele Fendrich, Wolfgang Jahnke, Doriano Fabbro

Blood (2011) 118 (21): 1674.

https://doi.org/10.1182/blood.V118.21.1674.1674

Published: 2011

Journal Articles

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRα, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

Blood (2010) 115 (21): 4206–4216.

https://doi.org/10.1182/blood-2009-11-251751

Published: 2010

Includes: Supplemental data

Journal Articles

Combination of the Hedgehog Pathway Inhibitor LDE225 and Nilotinib Eliminates Chronic Myeloid Leukemia Stem and Progenitor Cells.

David A Irvine, roMB, ChB, Bin Zhang, MD, PhD, Elaine K Allan, BSc, Tessa L Holyoake, PhD, MB, ChB, FRCP, FRCPath, FRSE, Marion Dorsch, PhD, Paul W Manley, PhD, Ravi Bhatia, MD, PhD, Mhairi Copland, PhD, BSc, MB, ChB, MRCP, FRCPath

Blood (2009) 114 (22): 1428.

https://doi.org/10.1182/blood.V114.22.1428.1428

Published: 2009

Journal Articles

Most CML patients who have a suboptimal response to imatinib have low OCT-1 activity: higher doses of imatinib may overcome the negative impact of low OCT-1 activity

Deborah L. White, Verity A. Saunders, Phuong Dang, Jane Engler, Amity Venables, Stephanie Zrim, Andrew Zannettino, Kevin Lynch, Paul W. Manley, Timothy Hughes

Blood (2007) 110 (12): 4064–4072.

https://doi.org/10.1182/blood-2007-06-093617

Published: 2007

Includes: Supplemental data

Journal Articles

Characterisation of Nilotinib Transport in Chronic Myeloid Leukaemia Cells.

Andrea Davies, PhD, Athina Giannoudis, PhD, Claire M. Lucas, BSc, Robert J. Harris, PhD, Paul W. Manley, PhD, Munir Pirmohamed, PhD, FRCP, FRCP(E), Richard E. Clark, MA, MD, FRCP, FRCPat

Blood (2007) 110 (11): 2364.

https://doi.org/10.1182/blood.V110.11.2364.2364

Published: 2007

Journal Articles

Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study

Arghya Ray, Sandra W. Cowan-Jacob, Paul W. Manley, Jürgen Mestan, James D. Griffin

Blood (2007) 109 (11): 5011–5015.

https://doi.org/10.1182/blood-2006-01-015347

Published: 2007

Includes: Supplemental data

Journal Articles

Imatinib increases the intracellular concentration of nilotinib, which may explain the observed synergy between these drugs

Deborah L. White, Verity A. Saunders, Steven R. Quinn, Paul W. Manley, Timothy P. Hughes

Blood (2007) 109 (8): 3609–3610.

https://doi.org/10.1182/blood-2006-11-058032

Published: 2007

Journal Articles

Synergistic Growth-Inhibitory Effects of Two Tyrosine Kinase Inhibitors, Dasatinib and PKC412, on Neoplastic Mast Cells Expressing the D816V-Mutated Oncogenic Variant of KIT.

Karoline V. Gleixner, MD, Matthias Mayerhofer, MD, Karoline Sonneck, MD, Alexander Gruze, Puchit Samorapoompichit, MD, Karl J. Aichberger, MD, Francis Y. Lee, PhD, Paul W. Manley, PhD, Doriano Fabbro, PhD, Winfried F. Pickl, MD, Christian Sillaber, MD, Peter Valent, MD

Blood (2006) 108 (11): 526.

https://doi.org/10.1182/blood.V108.11.526.526

Published: 2006

Journal Articles

Bcr-Abl Binding Modes of Dasatinib, Imatinib and Nilotinib: An NMR Study.

Paul W. Manley, Sandra W. Cowan-Jacob, Gabriele Fendrich, André Strauss, Navratna Vapai, Stephan Grzesiek, Wolfgang Jahnke

Blood (2006) 108 (11): 747.

https://doi.org/10.1182/blood.V108.11.747.747

Published: 2006

Journal Articles

Hemin Confers Resistance to Imatinib (Glivec)-Induced Cell Death but Enhances Nilotinib (AMN107) Cytotoxicity in Human K-562 CML Leukemia Cells.

Ioannis D. Bonovolias, Paul W. Manley, Asterios S. Tsiftsoglou

Blood (2006) 108 (11): 4769.

https://doi.org/10.1182/blood.V108.11.4769.4769

Published: 2006

Journal Articles

Imatinib (Glivec) and Nilotinib (AMN107), Two Selective Inhibitors of Bcr-Abl Tyrosine Kinase, Induce Hemoglobin Production in Human K-562 CML Erythroleukemia Cells in Addition To Promoting Apoptosis.

Asterios S. Tsiftsoglou, Paul W. Manley, Ioannis D. Bonovolias

Blood (2006) 108 (11): 4772.

https://doi.org/10.1182/blood.V108.11.4772.4772

Published: 2006

Journal Articles

Adaptive secretion of granulocyte-macrophage colony-stimulating factor (GM-CSF) mediates imatinib and nilotinib resistance in BCR/ABL + progenitors via JAK-2/STAT-5 pathway activation

Ying Wang, Dali Cai, Cornelia Brendel, Christine Barett, Philipp Erben, Paul W. Manley, Andreas Hochhaus, Andreas Neubauer, Andreas Burchert

Blood (2006) 109 (5): 2147–2155.

https://doi.org/10.1182/blood-2006-08-040022

Published: 2006

Includes: Supplemental data

Journal Articles

Adaptive Autocrine Secretion of the Granulocyte Macrophage Colony Stimulating Factor (GM-CSF) Mediates Imatinib- and Nilotinib-Resistance in BCR/ABL-Positive Progenitors Via JAK-2/STAT-5 Pathway Activation.

Andreas Burchert, Ying Wang, Cornelia Brendel, Philipp Erben, Paul W. Manley, Andreas Hochhaus, Dali Cai, Andreas Neubauer

Blood (2006) 108 (11): 2187.

https://doi.org/10.1182/blood.V108.11.2187.2187

Published: 2006

NARROW

Structural and Biochemical Studies Confirming the Mechanism of Action of Asciminib, an Agent Specifically Targeting the ABL Myristoyl Pocket (STAMP)

Comparison of the Profile of the AML Drug Midostaurin (Rydapt®) As a Kinase Inhibitor with Those of Its Predominant Primary Human Metabolites

ABL001, a Potent Allosteric Inhibitor of BCR-ABL, Prevents Emergence of Resistant Disease When Administered in Combination with Nilotinib in an in Vivo Murine Model of Chronic Myeloid Leukemia

Clinical and Preclinical Characterisation Of The Metabolites Of The BCR-ABL Tyrosine Kinase Inhibitor Nilotinib

Assessment of Clinical Safety and Estimate of Survival in Iraqi Patients with Chronic Myeloid Leukemia Switched From Glivec (β-Crystalline Form of Imatinib Mesylate) to an α-Crystalline Copy of Imatinib Mesylate

Potentiation of the Effects of Nilotinib by Combination with Plerixafor in a Mouse Model of BCR-ABL-Positive Residual Disease

Fingolimod (FTY720) Inhibits BCR-ABL Signaling Allosterically by Binding to the Myristate Binding Site

Nilotinib, in Comparison to Both Dasatinib and Imatinib, Possesses a Greatly Prolonged Residence Time When Bound to the BCR-ABL Kinase SH1 Domain

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRα, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

Combination of the Hedgehog Pathway Inhibitor LDE225 and Nilotinib Eliminates Chronic Myeloid Leukemia Stem and Progenitor Cells.

Most CML patients who have a suboptimal response to imatinib have low OCT-1 activity: higher doses of imatinib may overcome the negative impact of low OCT-1 activity

Characterisation of Nilotinib Transport in Chronic Myeloid Leukaemia Cells.

Identification of BCR-ABL point mutations conferring resistance to the Abl kinase inhibitor AMN107 (nilotinib) by a random mutagenesis study

Imatinib increases the intracellular concentration of nilotinib, which may explain the observed synergy between these drugs

Synergistic Growth-Inhibitory Effects of Two Tyrosine Kinase Inhibitors, Dasatinib and PKC412, on Neoplastic Mast Cells Expressing the D816V-Mutated Oncogenic Variant of KIT.

Bcr-Abl Binding Modes of Dasatinib, Imatinib and Nilotinib: An NMR Study.

Hemin Confers Resistance to Imatinib (Glivec)-Induced Cell Death but Enhances Nilotinib (AMN107) Cytotoxicity in Human K-562 CML Leukemia Cells.

Imatinib (Glivec) and Nilotinib (AMN107), Two Selective Inhibitors of Bcr-Abl Tyrosine Kinase, Induce Hemoglobin Production in Human K-562 CML Erythroleukemia Cells in Addition To Promoting Apoptosis.

Adaptive secretion of granulocyte-macrophage colony-stimulating factor (GM-CSF) mediates imatinib and nilotinib resistance in BCR/ABL + progenitors via JAK-2/STAT-5 pathway activation

Adaptive Autocrine Secretion of the Granulocyte Macrophage Colony Stimulating Factor (GM-CSF) Mediates Imatinib- and Nilotinib-Resistance in BCR/ABL-Positive Progenitors Via JAK-2/STAT-5 Pathway Activation.

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American Society of Hematology

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American Society of Hematology

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